Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C24H22N4O3 |
| Molecular Weight | 414.4565 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C=CC(=C1)C(N)=O)N2C(CCC(O)=O)=CC=C2C3=CC=C(C=C3)N4C=CN=C4
InChI
InChIKey=YVPGZQLRPAGKLA-UHFFFAOYSA-N
InChI=1S/C24H22N4O3/c1-16-14-18(24(25)31)4-9-21(16)28-20(8-11-23(29)30)7-10-22(28)17-2-5-19(6-3-17)27-13-12-26-15-27/h2-7,9-10,12-15H,8,11H2,1H3,(H2,25,31)(H,29,30)
DescriptionCurator's Comment: Description was created using several sources including:
https://www.ncbi.nlm.nih.gov/pubmed/22335564 | https://www.ncbi.nlm.nih.gov/pubmed/24405692 | http://ir.nivalis.com/press-releases/detail/12/n30-pharmaceuticals-announces-first-patient-treated-in
Curator's Comment: Description was created using several sources including:
https://www.ncbi.nlm.nih.gov/pubmed/22335564 | https://www.ncbi.nlm.nih.gov/pubmed/24405692 | http://ir.nivalis.com/press-releases/detail/12/n30-pharmaceuticals-announces-first-patient-treated-in
N6022 is a novel, first-in-class drug with potent reversible inhibitory activity against S-nitrosoglutathione reductase (GSNOR) and a potential agent for the treatment of acute asthma and cystic fibrosis (CF). Decreased levels of GSNO in the lungs of asthmatics and cystic fibrosis patients have been attributed to increased GSNO catabolism via GSNO reductase (GSNOR) leading to loss of GSNO- and NO- mediated bronchodilatory and anti-inflammatory actions. N6022 restore GSNO levels by inhibiting GSNOR. Inhibition of GSNOR by N6022 has shown safety and efficacy in animal models of asthma, chronic obstructive pulmonary disease, and inflammatory bowel disease. N6022 reduced bronchoconstriction and pulmonary inflammation in a mouse model of asthma. The significant bronchodilatory and anti-inflammatory actions of N6022 in the airways are consistent with restoration of GSNO levels through GSNOR inhibition.
Originator
Approval Year
Doses
| Dose | Population | Adverse events |
|---|---|---|
5 mg 1 times / day multiple, intravenous Studied dose Dose: 5 mg, 1 times / day Route: intravenous Route: multiple Dose: 5 mg, 1 times / day Sources: Page: p.326 |
unhealthy, 32.9 n = 14 Health Status: unhealthy Condition: Asthma Age Group: 32.9 Sex: M+F Population Size: 14 Sources: Page: p.326 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Discovery of s-nitrosoglutathione reductase inhibitors: potential agents for the treatment of asthma and other inflammatory diseases. | 2011 May 12 |
|
| A nonclinical safety and pharmacokinetic evaluation of N6022: a first-in-class S-nitrosoglutathione reductase inhibitor for the treatment of asthma. | 2012 Feb |
|
| Mechanism of inhibition for N6022, a first-in-class drug targeting S-nitrosoglutathione reductase. | 2012 Mar 13 |
|
| Pharmacologic inhibition of S-nitrosoglutathione reductase protects against experimental asthma in BALB/c mice through attenuation of both bronchoconstriction and inflammation. | 2014 Jan 10 |
Sample Use Guides
A 5 mg single dose given intravenously via syringe pump over 1 minute.
Route of Administration:
Intravenous
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SUBSTANCE RECORD
